How can micelle systems be rebuilt by a heating process?

Area of Science:

• Pharmaceutical Sciences
• Mycology
• Biochemistry

Background:

• Aqueous micellar systems of Amphotericin B (AmB) and sodium deoxycholate (DOC) are crucial for treating systemic fungal infections.
• Understanding the stability and properties of these micelles after heat treatment is essential for optimizing drug delivery and safety.

Purpose of the Study:

• To evaluate the physicochemical and pharmacotoxicological properties of an aqueous micellar system of Amphotericin B and sodium deoxycholate after heat treatment.
• To assess the efficacy and safety of the heat-treated (AmB-DOC-H) versus unheated (AmB-DOC) micellar systems in vitro.

Main Methods:

• Heated (AmB-DOC-H) and unheated (AmB-DOC) micelles were prepared and diluted to various concentrations.
• Physicochemical studies included spectral analysis.
• Pharmacotoxicity and efficacy assays used human red blood cells (RBC) and Candida parapsilosis (Cp) models, assessing K+ leakage, hemoglobin leakage, and cell survival.

Main Results:

• Spectral analysis showed a shift in the AmB-DOC aggregate peak from 327 nm to 323 nm for AmB-DOC-H.
• AmB-DOC-H exhibited significantly lower hemoglobin leakage from RBC compared to AmB-DOC at high concentrations.
• Both AmB-DOC and AmB-DOC-H demonstrated similar K+ leakage profiles and comparable antifungal activity against Cp.

Conclusions:

• Heat treatment effectively modifies the Amphotericin B-sodium deoxycholate micellar system, resulting in reduced toxicity.
• The heat-treated system (AmB-DOC-H) retains significant antifungal efficacy comparable to the unheated system.
• This novel procedure presents a simple, cost-effective, and safer method for producing improved micellar systems for systemic fungal infection treatment.